oxadiazoles and oxolamine

Topics: Aged; Antitussive Agents; Capsaicin; Cough; Cross-Over Studies; Female; Humans; Male; Middle Aged; Oxadiazoles; Pilot Projects; Pulmonary Disease, Chronic Obstructive; Respiratory Function Tests; Single-Blind Method

A single-blind, between-patients trial was run to compare the fluidifying, expectorant, antitussive, antipyretic and anti-inflammatory activity, and the local and systemic tolerance of guacetisal, an active principle obtained by the esterification of acetylsalicylic acid and guaiacol, and oxolamine phosphate, in which the suspension formulation for adults was administered to 30 presenile and senile patients of both sexes with chronic obstructive bronchopathy. A higher activity on the part of guacetisal was noted. The results obtained are illustrated and discussed.

Topics: Aged; Aspirin; Clinical Trials as Topic; Female; Humans; Lung Diseases, Obstructive; Male; Middle Aged; Oxadiazoles; Respiration

The possible reason for the significantly greater AUC of oral warfarin with oral oxolamine in male Sprague-Dawley rats was evaluated. After oral administration of warfarin at a dose of 2 mg/kg to male rats with oxolamine at doses of 10 and 50 mg/kg, the AUC values of warfarin were significantly greater than the controls (254 and 330 versus 180 microg h/ml). However, the AUC values of warfarin were not affected by oxolamine in female rats. This could be due to inhibition of CYP2B1, 2C11 and 3A2 by oxolamine in male rats, since warfarin was metabolized via CYP1A1, 2B1, 2C6, 2C11 and 3A2 in rats and CYP2B1 is male dominant, and CYP2C11 and 3A2 are male specific. Therefore, phenytoin, torasemide and clarithromycin (mainly metabolized via CYP2B1/2, 2C11 and 3A2 in rats, respectively) were administered intravenously to male rats with or without oral oxolamine. After oral oxolamine at doses of 10 and 50 mg/kg, the AUC of phenytoin was significantly greater (1280 and 1640 versus 938 microg min/ml), however, the AUC values of torasemide and clarithromycin were independent of oxolamine. The above data suggest that the significantly greater AUC of oral warfarin with oral oxolamine could be due to inhibition of CYP2B1/2 by oxolamine in male rats.

Topics: Administration, Oral; Animals; Anti-Inflammatory Agents, Non-Steroidal; Anticoagulants; Area Under Curve; Clarithromycin; Cytochrome P-450 CYP2B1; Cytochrome P-450 Enzyme System; Dose-Response Relationship, Drug; Drug Interactions; Female; Male; Oxadiazoles; Phenytoin; Protein Binding; Rats; Rats, Sprague-Dawley; Sex Factors; Sulfonamides; Torsemide; Warfarin

Topics: Adult; Aged; Aged, 80 and over; Anti-Inflammatory Agents, Non-Steroidal; Anticoagulants; Drug Interactions; Female; Humans; International Normalized Ratio; Middle Aged; Oxadiazoles; Prospective Studies; Warfarin

Twenty reports in Australia, Belgium and The Netherlands have implicated oxolamine-citrate cough-mixtures as a cause of hallucinations in children of less than 10 years of age. Fever is not thought to be a likely alternative explanation. Similar reactions in older children and adults have not been reported and it is possible that the recommended doses for young children are too high. Information about the use of the drug in Australia suggests that such reactions are uncommon, but the information should be interpreted cautiously.

Topics: Antitussive Agents; Child; Child, Preschool; Female; Hallucinations; Humans; Infant; Male; Oxadiazoles

Topics: Acute Disease; Administration, Oral; Adolescent; Adult; Anti-Inflammatory Agents; Antitussive Agents; Bronchitis; Female; Humans; Male; Oxadiazoles; Tracheitis

Topics: Anti-Inflammatory Agents; Antitussive Agents; Humans; Oxadiazoles; Respiratory System; Respiratory Tract Infections; Tuberculosis; Tuberculosis, Pulmonary

Topics: Analgesics; Analgesics, Non-Narcotic; Anti-Inflammatory Agents; Antipyretics; Expectorants; Inflammation; Mice; Oxadiazoles; Research; Respiratory Tract Infections; Tetracycline

Topics: Antitussive Agents; Bronchial Diseases; Bronchitis; Bronchopneumonia; Hemopneumothorax; Humans; Influenza, Human; Lung Diseases; Oxadiazoles; Pleurisy; Pneumonia; Pneumonia, Viral; Respiratory Tract Infections; Tetracycline

Topics: Analgesics; Analgesics, Non-Narcotic; Antipyretics; Antitussive Agents; Cats; Chemistry, Pharmaceutical; Guinea Pigs; Hydroxylation; Metabolism; Mice; Oxadiazoles; Pharmacology; Research

Topics: Antitussive Agents; Bronchitis; Humans; Oxadiazoles; Respiratory System; Respiratory Tract Diseases; Tetracycline; Tuberculosis; Tuberculosis, Pulmonary

Topics: Adolescent; Anti-Inflammatory Agents; Antitussive Agents; Asthma; Child; Common Cold; Cough; Oxadiazoles; Rhinitis, Allergic, Seasonal; Toxicology

Topics: Anti-Inflammatory Agents; Biomedical Research; Child; Drug Therapy; Humans; Infant; Inflammation; Oxadiazoles; Oxazoles; Pediatrics; Toxicology

Topics: Aminopyrine; Analgesics; Analgesics, Non-Narcotic; Antipyretics; Bronchitis; Child; Humans; Muscle Relaxants, Central; Otitis; Oxadiazoles; Pediatrics; Pharyngitis; Sulfamethoxypyridazine; Tonsillitis; Tracheitis

Topics: Antitussive Agents; Bronchial Diseases; Geriatrics; Humans; Laryngectomy; Oxadiazoles; Protein Synthesis Inhibitors; Tetracycline

Topics: Antitussive Agents; Humans; Oxadiazoles; Pharmacology; Respiratory Function Tests; Silicosis

Topics: Analgesics; Analgesics, Non-Narcotic; Anti-Bacterial Agents; Antibiotics, Antitubercular; Antipyretics; Antitussive Agents; Asthma; Bronchitis; Bronchopneumonia; Cough; Humans; Oxadiazoles

Topics: Analgesics; Analgesics, Non-Narcotic; Antipyretics; Geriatrics; Oxadiazoles

Topics: Bronchitis; Cough; Disease; Humans; Inflammation; Oxadiazoles; Trachea

Topics: Cough; Oxadiazoles

Topics: Antitussive Agents; Asthma; Bronchitis; Dyspnea; Oxadiazoles

Topics: Antitussive Agents; Humans; Inflammation; Oxadiazoles; Respiratory System; Respiratory Tract Infections; Tetracycline

Topics: Analgesics; Analgesics, Non-Narcotic; Antipyretics; Bronchitis; Bronchopneumonia; Child; Cough; Infant; Measles; Oxadiazoles

Topics: Analgesics; Analgesics, Non-Narcotic; Antipyretics; Cough; Hospitals; Oxadiazoles

Topics: Animals; Azoles; Humans; Inflammation; Oxadiazoles; Rats

Topics: Anti-Inflammatory Agents; Cough; Humans; Inflammation; Oxadiazoles

Topics: Cough; Inflammation; Oxadiazoles

Topics: Carbonic Anhydrases; Cough; Humans; Oxadiazoles; Prothrombin; Prothrombin Time; Tuberculosis; Tuberculosis, Pulmonary

Topics: Bronchitis; Cough; Humans; Oxadiazoles; Recurrence

Topics: Cough; Humans; Oxadiazoles

Topics: Cough; Humans; Oxadiazoles

Topics: Asthma; Cough; Humans; Oxadiazoles; Syndrome

Topics: Bronchitis; Bronchitis, Chronic; Cough; Humans; Oxadiazoles

Topics: Antitussive Agents; Cough; Humans; Oxadiazoles

Topics: Cough; Humans; Oxadiazoles

Topics: Cough; Humans; Oxadiazoles

Topics: Aged; Aged, 80 and over; Aging; Bronchitis; Cough; Humans; Oxadiazoles

Topics: Bronchitis; Child; Cough; Humans; Infant; Oxadiazoles; Pediatrics